Výsledky vyhledávání - "EGFR-INHIBITION"

Akademický článek

New 1,2,3-triazole/1,2,4-triazole hybrids linked to oxime moiety as nitric oxide donor selective COX-2, aromatase, B-RAFV600E and EGFR inhibitors celecoxib analogs: design, synthesis, anti-inflammatory/anti-proliferative activities, apoptosis and molecular modeling study

Autor: Wael A. A. Fadaly, Mohamed T. M. Nemr, Taha H. Zidan, Fatma E. A. Mohamed, Marwa M. Abdelhakeem, Nour N. Abu Jayab, Hany A. Omar, Khaled R. A. Abdellatif

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 38, Iss 1 (2023)

A new series of bis-triazole 19a-l was synthesised for the purpose of being hybrid molecules with both anti-inflammatory and anti-cancer activities and assessed for cell cycle arrest, NO release. Compounds 19c, 19f, 19h, 19 l exhibited COX-2 selectiv

Externí odkaz: https://doaj.org/article/6ddb10d4238d42518a92a6f21fd82cea

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Akademický článek

New pyrazolyl-thiazolidinone/thiazole derivatives as celecoxib/dasatinib analogues with selective COX-2, HER-2 and EGFR inhibitory effects: design, synthesis, anti-inflammatory/anti-proliferative activities, apoptosis, molecular modelling and ADME studies

Autor: Wael A. A. Fadaly, Taha H. Zidan, Nesma M. Kahk, Fatma E. A. Mohamed, Marwa M. Abdelhakeem, Rehab G. Khalil, Mohamed T. M. Nemr

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 38, Iss 1 (2023)

Two new series of pyrazolyl-thiazolidinone/thiazole derivatives 16a–b and 18a–j were synthesised, merging the scaffolds of celecoxib and dasatinib. Compounds 16a, 16b and 18f inhibit COX-2 with S.I. 134.6, 26.08 and 42.13 respectively (celecoxib

Externí odkaz: https://doaj.org/article/6fc6d76d93e9492182ddccc004eb8ea8

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Akademický článek

Recruitment of hexahydroquinoline as anticancer scaffold targeting inhibition of wild and mutants EGFR (EGFRWT, EGFRT790M, and EGFRL858R)

Autor: Mahmoud G. Abo Al-Hamd, Haytham O. Tawfik, Omeima Abdullah, Koki Yamaguchi, Masaharu Sugiura, Ahmed B. M. Mehany, Mervat H. El-Hamamsy, Tarek F. El-Moselhy

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 38, Iss 1 (2023)

Hexahydroquinoline (HHQ) scaffold was constructed and recruited for development of new series of anticancer agents. Thirty-two new compounds were synthesised where x-ray crystallography was performed to confirm enantiomerism. Thirteen compounds showe

Externí odkaz: https://doaj.org/article/9056c1dbec114abe9db25e676a2af1f4

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Akademický článek

Design and synthesis of novel quinazolinone-based derivatives as EGFR inhibitors with antitumor activity

Autor: Amr Sonousi, Rasha A. Hassan, Eman O. Osman, Amr M. Abdou, Soha H. Emam

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 2644-2659 (2022)

Nineteen new quinazolin-4(3H)-one derivatives 3a–g and 6a–l were designed and synthesised to inhibit EGFR. The antiproliferative activity of the synthesised compounds was tested in vitro against 60 different human cell lines. The most potent comp

Externí odkaz: https://doaj.org/article/e43d0eca47954f19a7dcf20e80e8a8de

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Akademický článek

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Akademický článek

Tumor necrosis factor in lung cancer: Complex roles in biology and resistance to treatment

Autor: Ke Gong, Gao Guo, Nicole Beckley, Yue Zhang, Xiaoyao Yang, Mishu Sharma, Amyn A. Habib

Publikováno v: Neoplasia: An International Journal for Oncology Research, Vol 23, Iss 2, Pp 189-196 (2021)

Tumor necrosis factor (TNF) and its receptors are widely expressed in non-small cell lung cancer (NSCLC). TNF has an established role in inflammation and also plays a key role in inflammation-induced cancer. TNF can induce cell death in cancer cells

Externí odkaz: https://doaj.org/article/16a3431681c94e9a972b70c8c2fd9d68

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Akademický článek

Synthesis, potential antitumor activity, cell cycle analysis, and multitarget mechanisms of novel hydrazones incorporating a 4-methylsulfonylbenzene scaffold: a molecular docking study

Autor: Alaa A.-M. Abdel-Aziz, Adel S. El-Azab, Nawaf A. AlSaif, Ahmad J. Obaidullah, Abdulrahman M. Al-Obaid, Ibrahim A. Al-Suwaidan

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 1520-1538 (2021)

Hydrazone is a bioactive pharmacophore that can be used to design antitumor agents. We synthesised a series of hydrazones (compounds 4–24) incorporating a 4-methylsulfonylbenzene scaffold and analysed their potential antitumor activity. Compounds 6

Externí odkaz: https://doaj.org/article/f2cef13a3c0140699e1966145b1894a6

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Akademický článek

Real-world Treatment Patterns and Outcomes with Systemic Therapies in Unresectable Locally Advanced and Metastatic Cutaneous Squamous Cell Carcinoma in Germany

Autor: Felix Kramb, Christoph Doerfer, Andreas Meiwes, Karthik Ramakrishnan, Thomas Eigentler, Claus Garbe, Ulrike Keim, Ulrike Leiter

Publikováno v: Acta Dermato-Venereologica, Vol 102 (2022)

Advanced cutaneous squamous cell carcinoma is a challenge to treat. Conventional systemic treatment options include chemotherapy and epidermal growth factor receptor-inhibitors. The aim of this study was to assess clinical outcomes with systemic trea

Externí odkaz: https://doaj.org/article/7fb27b628fe74e17a7947ab978c9790b

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